EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC 50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1 , significantly down-regulating the expression of HOXA9 and MEIS1 . EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis ( apoptosis ) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.
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